TABLE 3.
Effect of epoxyketone and vinyl sulfone on residual survival
HeLa S3 cells were treated with inhibitors at the concentrations indicated (or mock-treated) for 24 h. Cells were harvested in fresh media and replated in fresh media on 6-well plates at densities varying from 50,000 to 100,000 cells/well. 21 days after plating, media were removed; colonies were washed with PBS, stained with methylene blue, and counted. Numbers are averages ± S.E. of two independent experiments.
| Concentration | Colonies | Active site |
||
|---|---|---|---|---|
| β5 | β1 | β2 | ||
| μm | % control | % inhibition | ||
| NC-005 | ||||
| 1 | 0.12 ± 0.11 | 98.7 ± 0.05 | 65 ± 1 | 69 ± 1 |
| 3 | 0 | 99.0 ± 0.05 | 84 ± 1 | 88 ± 1 |
| NC-005-pvs | ||||
| 3 | 2.35 ± 1.77 | 98.3 ± 0 | 39 ± 5 | 16 ± 8 |
| 9 | 0.72 ± 0.13 | 98.4 ± 0.05 | 46 ± 0.25 | 20 ± 1 |